Please can you help me how to prepare tablets with sorbitol, xylitol and magnesium stearate with oil-ethanol AIP (2,5 % w/w)? How to mix all ingredients to get homogenous mixture for tableting? Thank you very much.
Certainly! Here's a guide on how to prepare tablets with sorbitol, xylitol, magnesium stearate, and oil-ethanol AIP (Active Ingredient Powder), ensuring a homogeneous mixture for tableting.
Ingredients: Sorbitol: Used as a filler or bulking agent. Xylitol: Another sugar alcohol that may be used for sweetness or as a bulking agent. Magnesium Stearate: A lubricant that helps with the flow properties of the powder and reduces friction during tableting. Oil-Ethanol AIP (2.5% w/w): The active ingredient (AIP) dissolved in an oil-ethanol solution (2.5% weight/weight). This is the active substance that will be incorporated into the tablets. Steps to Prepare Tablets: 1. Prepare the Oil-Ethanol AIP Solution Weigh out the required amount of AIP (based on your formulation's final dose) to achieve a concentration of 2.5% w/w in the solution. Dissolve the AIP in a mixture of oil and ethanol. The ethanol helps dissolve the AIP, and the oil ensures that the AIP remains suspended. Mix thoroughly and ensure the solution is homogeneous. 2. Blend Sorbitol and Xylitol Weigh the required amounts of sorbitol and xylitol, based on the desired tablet weight and formulation. Blend sorbitol and xylitol in a dry state to achieve a uniform distribution. This is typically done using a powder mixer or v-blender. The goal here is to have a homogeneous mixture of sorbitol and xylitol before the introduction of any liquids. 3. Incorporate the Oil-Ethanol AIP Solution Slowly add the oil-ethanol AIP solution to the dry powder blend (sorbitol and xylitol) in small portions. The key is to avoid clumping or uneven distribution of the active ingredient. Mix thoroughly to ensure the AIP solution is evenly distributed throughout the powder blend. You can use a planetary mixer or a paddle mixer for this step. If the mixture becomes too wet, allow it to dry slightly before proceeding, but be careful not to dry it out completely. 4. Add Magnesium Stearate (Lubrication) Weigh the appropriate amount of magnesium stearate (usually around 0.5-2% of the total mixture weight). Blend the magnesium stearate into the powder mixture gently. Overmixing magnesium stearate can cause it to act as a lubricant, reducing tablet cohesion, so mix only until it's uniformly distributed. 5. Granulation (if necessary) If your mixture is too fine or you need to improve flow properties, you may need to perform dry granulation. This involves compressing the mixture into larger particles or granules to improve its compressibility and flow. Alternatively, if the mixture is too dry, wet granulation with a small amount of water or ethanol might be necessary before adding the lubricant. 6. Compress into Tablets Once the final mixture is homogeneous, it’s ready for compression into tablets using a tablet press. Adjust the tablet press settings to get the desired tablet weight and hardness. 7. Post-Compression (Drying, if needed) If necessary, after compression, allow the tablets to dry (if there is residual ethanol or moisture) in a drying oven or under ambient conditions to ensure they’re dry enough for storage. Tips for Homogeneous Mixing: Ensure the ingredients are well-mixed at each step, especially when incorporating the oil-ethanol AIP solution. Inadequate mixing could lead to uneven distribution of the active ingredient. Consider using blending equipment like a high-shear mixer or twin-screw blender for larger batches to ensure uniformity. Avoid excessive mixing with magnesium stearate to prevent it from affecting tablet hardness. During the granulation phase, ensure you’re achieving the right consistency to improve tabletability.
By following these steps, you should be able to produce a homogeneous mixture for tableting.
Tereza Feglarová, To prepare tablets containing sorbitol, xylitol, magnesium stearate, and a liquid oil-ethanol AIP (2.5% w/w), a liquid adsorption technique is recommended to ensure a homogeneous and compressible mixture.
First, sieve all solid excipients (sorbitol, xylitol) to ensure uniform particle size. Prepare the oil-ethanol AIP by dissolving or dispersing the active ingredient uniformly. To incorporate this liquid into the tablet blend, slowly adsorb the AIP onto sorbitol and/or xylitol using a suitable mixer (e.g., planetary or high-shear mixer). Add the liquid gradually (dropwise or spray) under continuous mixing to prevent localized wet spots. The goal is to fully absorb the liquid into the powder without making it sticky or wet.
If the mixture feels damp or retains ethanol, dry the blend using a tray dryer (40–50°C) or vacuum oven until ethanol content is within acceptable limits. Once dry, sieve the mass through a #20–30 mesh to obtain free-flowing granules.
After drying and sizing, add magnesium stearate (typically 0.25–1% w/w) as a lubricant. Mix gently for 1–3 minutes to avoid over-lubrication, which can reduce tablet hardness and delay disintegration.
Finally, compress the blend into tablets using standard tooling. If the oil load is high, consider adding adsorbents like colloidal silicon dioxide to improve powder flow and reduce oil migration.
This approach ensures a uniform and compressible powder blend, even with liquid components, and minimizes issues like sticking or poor disintegration.